EP2817295A4 - Substituierte 5-aminothieno-[2,3-c-]pyridazin-6-carboxamidanaloga als positive allosterische modulatoren des muskarinacetylcholinrezeptors m4 - Google Patents
Substituierte 5-aminothieno-[2,3-c-]pyridazin-6-carboxamidanaloga als positive allosterische modulatoren des muskarinacetylcholinrezeptors m4Info
- Publication number
- EP2817295A4 EP2817295A4 EP13751391.7A EP13751391A EP2817295A4 EP 2817295 A4 EP2817295 A4 EP 2817295A4 EP 13751391 A EP13751391 A EP 13751391A EP 2817295 A4 EP2817295 A4 EP 2817295A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- aminothieno
- pyridazine
- substituted
- acetylcholine receptor
- positive allosteric
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- FDZZBIMAFOTVMT-UHFFFAOYSA-N 5-aminothieno[2,3-c]pyridazine-6-carboxamide Chemical class N1=CC=C2C(N)=C(C(=O)N)SC2=N1 FDZZBIMAFOTVMT-UHFFFAOYSA-N 0.000 title 1
- 102000000413 Muscarinic acetylcholine receptor M4 Human genes 0.000 title 1
- 108050008897 Muscarinic acetylcholine receptor M4 Proteins 0.000 title 1
- 230000003281 allosteric effect Effects 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP17199020.3A EP3321257A1 (de) | 2012-02-23 | 2013-02-23 | Substituierte 5-aminothieno-[2,3-c-]pyridazin-6-carboxamidanaloga als positive allosterische modulatoren des muskarinacetylcholinrezeptors m4 |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261602481P | 2012-02-23 | 2012-02-23 | |
PCT/US2013/027534 WO2013126856A1 (en) | 2012-02-23 | 2013-02-23 | Substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP17199020.3A Division EP3321257A1 (de) | 2012-02-23 | 2013-02-23 | Substituierte 5-aminothieno-[2,3-c-]pyridazin-6-carboxamidanaloga als positive allosterische modulatoren des muskarinacetylcholinrezeptors m4 |
Publications (3)
Publication Number | Publication Date |
---|---|
EP2817295A1 EP2817295A1 (de) | 2014-12-31 |
EP2817295A4 true EP2817295A4 (de) | 2015-08-26 |
EP2817295B1 EP2817295B1 (de) | 2017-11-01 |
Family
ID=49006287
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP17199020.3A Withdrawn EP3321257A1 (de) | 2012-02-23 | 2013-02-23 | Substituierte 5-aminothieno-[2,3-c-]pyridazin-6-carboxamidanaloga als positive allosterische modulatoren des muskarinacetylcholinrezeptors m4 |
EP13751391.7A Active EP2817295B1 (de) | 2012-02-23 | 2013-02-23 | Substituierte 5-aminothieno-[2,3-c-]pyridazin-6-carboxamidanaloga als positive allosterische modulatoren des muskarinacetylcholinrezeptors m4 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP17199020.3A Withdrawn EP3321257A1 (de) | 2012-02-23 | 2013-02-23 | Substituierte 5-aminothieno-[2,3-c-]pyridazin-6-carboxamidanaloga als positive allosterische modulatoren des muskarinacetylcholinrezeptors m4 |
Country Status (4)
Country | Link |
---|---|
US (2) | US9493481B2 (de) |
EP (2) | EP3321257A1 (de) |
ES (1) | ES2656972T3 (de) |
WO (1) | WO2013126856A1 (de) |
Families Citing this family (44)
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EP2491038B1 (de) | 2009-10-23 | 2016-04-06 | Janssen Pharmaceutica N.V. | Disubstituierte octahy-dropyrrolo [3,4-c]pyrrole als orexinrezeptormodulatoren |
PE20140011A1 (es) | 2010-09-03 | 2014-01-31 | Forma Tm Llc | Compuestos y composiciones novedosos para la inhibicion de nampt |
US9586962B2 (en) * | 2011-04-20 | 2017-03-07 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators |
WO2013126856A1 (en) * | 2012-02-23 | 2013-08-29 | Vanderbilt University | Substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
WO2014149819A1 (en) | 2013-03-14 | 2014-09-25 | Kalyra Pharmaceuticals, Inc. | Bicyclic analgesic compounds |
WO2015027214A1 (en) | 2013-08-23 | 2015-02-26 | Vanderbilt University | Substituted thieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
WO2015089170A1 (en) | 2013-12-12 | 2015-06-18 | Kalyra Pharmaceuticals, Inc. | Bicyclic alkyl compounds and synthesis |
CN106232567B (zh) | 2014-03-07 | 2021-11-02 | 里科瑞尔姆Ip控股有限责任公司 | 螺桨烷衍生物及合成 |
CN106536518B (zh) * | 2014-05-19 | 2020-05-12 | 勃林格殷格翰动物保健美国公司 | 驱蠕虫化合物 |
US10308609B2 (en) | 2014-09-17 | 2019-06-04 | Zeno Royalties & Milestones, LLC | Bicyclic compounds |
WO2016179351A1 (en) | 2015-05-05 | 2016-11-10 | Northwestern University | Treatment of levodopa-induced dyskinesias |
EP3394061B1 (de) | 2015-12-23 | 2020-03-11 | Merck Sharp & Dohme Corp. | Allosterische 6,7-dihydro-5h-pyrrolo[3,4-b]pyridin-5-on-modulatoren des m4-muskarinischen acetylcholinrezeptors |
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CA2960253A1 (en) | 2016-03-10 | 2017-09-10 | Janssen Pharmaceutica Nv | Methods of treating depression using orexin-2 receptor antagonists |
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US10342782B2 (en) | 2016-07-27 | 2019-07-09 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor M4 |
BR112018007755A2 (pt) * | 2016-08-18 | 2018-10-23 | Univ Vanderbilt | moduladores alostéricos positivos do receptor muscarínico m4 de acetilcolina |
US10189857B2 (en) | 2016-09-13 | 2019-01-29 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor M4 |
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JP7099725B2 (ja) | 2016-11-07 | 2022-07-12 | ヴァンダービルト ユニヴァーシティ | ムスカリン性アセチルコリンレセプターm4のポジティブアロステリック調節因子 |
MA46899A (fr) | 2016-11-07 | 2021-04-14 | Univ Vanderbilt | Modulateurs allostériques positifs du récepteur muscarinique de l'acétylcholine m4 |
EP3534901B1 (de) | 2016-11-07 | 2022-06-22 | Vanderbilt University | Positive allosterische modulatoren des muskarinischen acetylcholinrezeptors m4 |
WO2018112842A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor |
WO2018112843A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
WO2018112840A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6, 5-fused heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
EP3366683A1 (de) | 2017-02-28 | 2018-08-29 | Acousia Therapeutics GmbH | Zyklische amide, acetamide und harnstoffe als kalium kanal öffner |
KR102296703B1 (ko) | 2017-03-20 | 2021-09-01 | 포르마 세라퓨틱스 인크. | 피루베이트 키나제 (pkr) 활성화제로서의 피롤로피롤 조성물 |
JP7157769B2 (ja) | 2017-05-15 | 2022-10-20 | リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー | 鎮痛剤化合物 |
US11065235B2 (en) | 2017-05-19 | 2021-07-20 | Council Of Scientific & Industrial Research | Substituted methanopyrido [2, 1-a] isoindolones as mAChR modulators for treating various associated pathophysiological conditions and process for preparation thereof |
DK3642202T3 (da) | 2017-06-22 | 2023-01-30 | Pfizer | Dihydro-pyrrolo-pyridin-derivater |
WO2019000236A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
WO2019000237A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
WO2019000238A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
EP3704126A4 (de) | 2017-11-03 | 2020-12-09 | Université de Montréal | Verbindungen und verwendung davon in der expansion von stammzellen und/oder vorläuferzellen |
TW201930311A (zh) | 2017-12-05 | 2019-08-01 | 泛德比爾特大學 | 蕈毒鹼型乙醯膽鹼受體m4之正向別構調節劑 |
US11376254B2 (en) | 2017-12-05 | 2022-07-05 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor M4 |
US20230055923A1 (en) | 2018-09-19 | 2023-02-23 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
BR112021005188A2 (pt) | 2018-09-19 | 2021-06-08 | Forma Therapeutics, Inc. | tratamento de anemia falciforme com um composto de ativação de piruvato cinase r |
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CN115246842B (zh) * | 2022-06-15 | 2024-05-24 | 深圳湾实验室 | 一类靶向去泛素化酶usp25和usp28的小分子抑制剂 |
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WO2013126856A1 (en) | 2012-02-23 | 2013-08-29 | Vanderbilt University | Substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
WO2014035829A1 (en) | 2012-08-31 | 2014-03-06 | Vanderbilt University | Substituted 3-aminothieno[2,3-c]pyridine-2-carboxamide analogs as positive allosteric modulators |
WO2015027214A1 (en) | 2013-08-23 | 2015-02-26 | Vanderbilt University | Substituted thieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
US20160200733A1 (en) | 2013-08-23 | 2016-07-14 | Vanderbilt University | Substituted thieno[2,3-b]pyridine-2-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
-
2013
- 2013-02-23 WO PCT/US2013/027534 patent/WO2013126856A1/en active Application Filing
- 2013-02-23 EP EP17199020.3A patent/EP3321257A1/de not_active Withdrawn
- 2013-02-23 US US14/380,659 patent/US9493481B2/en active Active
- 2013-02-23 EP EP13751391.7A patent/EP2817295B1/de active Active
- 2013-02-23 ES ES13751391.7T patent/ES2656972T3/es active Active
-
2016
- 2016-10-03 US US15/283,508 patent/US9868746B2/en active Active
Non-Patent Citations (12)
Title |
---|
A. E. BRADY ET AL: "Centrally Active Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Rats", JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol. 327, no. 3, 5 September 2008 (2008-09-05), pages 941 - 953, XP055081736, ISSN: 0022-3565, DOI: 10.1124/jpet.108.140350 * |
ABBADY, M. S. ET AL: "Synthesis and some reactions of thieno[2,3-c]pyridazine derivatives and their antibacterial activity", PHOSPHORUS, SULFUR AND SILICON AND THE RELATED ELEMENTS, vol. 86, no. 1-4, 1994, pages 203 - 209, XP009184922, ISSN: 1042-6507, DOI: 10.1080/10426509408018405 * |
AL-KAMALI, AHMED S. N. ET AL: "Synthesis and antibacterial activity of some novel thieno[2,3-c]pyridazines using 3-amino-5-phenyl-2-ethoxycarbonylthieno[2,3- c]pyridazine as a starting material", ARABIAN JOURNAL OF CHEMISTRY, vol. 7, no. 5, 2014, pages 775 - 780, XP002741787, ISSN: 1878-5352, DOI: 10.1016/J.ARABJC.2010.12.020 * |
AL-KAMALI, AHMED S. N.: "Synthesis and reactions of some new thieno[2,3-C]pyridazine derivatives", PHOSPHORUS, SULFUR AND SILICON AND THE RELATED ELEMENTS, vol. 184, no. 7, 2009, pages 1812 - 1824, XP002741779, ISSN: 1042-6507, DOI: 10.1080/10426500802353213 * |
EL-DEAN, A. M. KAMAL ET AL: "Novel synthesis of thieno[2,3-c]pyridazine and pyrimido[4',5':4,5]thieno[2,3-c]pyridazine derivatives", PHOSPHORUS, SULFUR AND SILICON AND THE RELATED ELEMENTS, vol. 180, no. 2, 2005, pages 413 - 424, XP002741781, ISSN: 1042-6507, DOI: 10.1080/104265090509216 * |
GABER, ABD EL-AAL M. ET AL: "Synthesis of novel polyfunctionally substituted thieno[2,3-c]pyridazines", JOURNAL OF THE CHINESE CHEMICAL SOCIETY (TAIPEI, TAIWAN), vol. 51, no. 6, 2004, pages 1325 - 1331, XP002741783, ISSN: 0009-4536, DOI: 10.1002/JCCS.200400192 * |
J. PHILLIP KENNEDY ET AL: "Synthesis and Structure-Activity Relationships of Allosteric Potentiators of the M 4 Muscarinic Acetylcholine Receptor", CHEMMEDCHEM, vol. 4, no. 10, 5 October 2009 (2009-10-05), pages 1600 - 1607, XP055081738, ISSN: 1860-7179, DOI: 10.1002/cmdc.200900231 * |
RADWAN, SH. M. ET AL: "Synthesis of pyridazothienothiazine and pyrimidothienopyridazines", PHOSPHORUS, SULFUR AND SILICON AND THE RELATED ELEMENTS, vol. 164, 2000, pages 299 - 313, XP002741782, ISSN: 1042-6507, DOI: 10.1080/10426500008045255 * |
RADWAN, SH. M. ET AL: "Synthesis of pyrrolo[1",2":1',2']pyrazino[6',5':4,5]thieno[2,3- c]pyridazine derivatives and related pentacyclic heterocycles", PHOSPHORUS, SULFUR AND SILICON AND THE RELATED ELEMENTS , 89(1-4), 193-8 CODEN: PSSLEC; ISSN: 1042-6507, 1994, XP009184919, DOI: 10.1080/10426509408020449 10.1080/10426509408020449 * |
RADWAN, SH. M. ET AL: "Synthesis of some new pyrimidothienopyridazines and related heterocycles", JOURNAL OF THE CHINESE CHEMICAL SOCIETY (TAIPEI, TAIWAN), vol. 52, no. 2, 2005, pages 303 - 308, XP002741780, ISSN: 0009-4536, DOI: 10.1002/JCCS.200500046 * |
RADWAN, SH. M.: "Synthesis and reactions of some new heterocyclic compounds containing thieno[2,3-c]pyridazine moiety", PHOSPHORUS, SULFUR AND SILICON AND THE RELATED ELEMENTS , 163, 153-169 CODEN: PSSLEC; ISSN: 1042-6507, vol. 163, 2000, pages 153 - 169, XP008169735, ISSN: 1042-6507, DOI: 10.1080/10426500008046617 * |
See also references of WO2013126856A1 * |
Also Published As
Publication number | Publication date |
---|---|
WO2013126856A1 (en) | 2013-08-29 |
EP2817295A1 (de) | 2014-12-31 |
US9493481B2 (en) | 2016-11-15 |
ES2656972T3 (es) | 2018-03-01 |
US20170022216A1 (en) | 2017-01-26 |
US9868746B2 (en) | 2018-01-16 |
US20150018309A1 (en) | 2015-01-15 |
EP3321257A1 (de) | 2018-05-16 |
EP2817295B1 (de) | 2017-11-01 |
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